Abstract: CXC chemokine receptor type 4(CXCR4) and its ligand(CXCL12) exerts crucial influence in regulating tumor growth, angiogenesis and metastasis. Studies show that the downstream signaling pathway can be activated by interaction of the chemokine receptor and its ligand to promote tumor growth and angiogenesis. Additional observation suggests that neoplastic tissue expresses high levels of CXCR4, and the site of tumor metastasis over expresses CXCL12, through which this specific binding ability can induce tumor metastasis. Thus, the CXCR4 levels could be used as a predictive marker of metastatic potential. Hopefully, the non-invasive imaging methods, such as SPECT/CT, PET, are employed in the imaging of the chemokine receptors to diagnose and treat the tumors in the early stage.